Indolinone derivative compounds that act as EWS-FLI1 transcription factor inhibitors are provided. Also provided are pharmaceutical compositions of the indolinone derivatives, methods of synthesizing the same, methods of treating using same, and assays for identifying the inhibitors of EWS-FLI1 oncoprotein.本發明提供充當EWS-FLI1轉錄因子抑制劑之吲哚啉酮衍生化合物。亦提供該等吲哚啉酮衍生物之醫藥組合物、其合成方法、使用其之治療方法及用於鑑別EWS-FLI1癌蛋白的抑制劑之分析。